HUP0302173A2 - Pyrazole compounds useful as protein kinase inhibitors - Google Patents

Pyrazole compounds useful as protein kinase inhibitors

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Publication number
HUP0302173A2
HUP0302173A2 HU0302173A HUP0302173A HUP0302173A2 HU P0302173 A2 HUP0302173 A2 HU P0302173A2 HU 0302173 A HU0302173 A HU 0302173A HU P0302173 A HUP0302173 A HU P0302173A HU P0302173 A2 HUP0302173 A2 HU P0302173A2
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Hungary
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group
atom
ring
condensed
unsaturated
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HU0302173A
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Hungarian (hu)
Inventor
David Bebbington
Robert Davies
Cornelia Forester
David Kay
Ronald Knegtel
Pan Li
Albert Pierce
Marion W. Wannamaker
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Vertex Pharmaceuticals Incorporated
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Application filed by Vertex Pharmaceuticals Incorporated filed Critical Vertex Pharmaceuticals Incorporated
Publication of HUP0302173A2 publication Critical patent/HUP0302173A2/en

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Abstract

A találmány a proteinkináz, különösen GSK-3 és Aurora-2 proteinkinázinhibitorokként funkcionáló általános képletű vegyületekre - amelyekképletében C gyűrű fenil-, piridil-, pirimidinil-, piridazinil-,pirazinil- vagy 1,2,4-triazinilcsoport, ahol a C gyűrű egy vagy két -R1 orto-szubsztituenst hordoz, a C gyűrűn lévő bármely más szénpozíció-R5 csoporttal szubsztituált, és adott esetben a C gyűrűn lévő kétszomszédos szubsztituens a közöttük lévő atomokkal együtt egykondenzált, telítetlen vagy részlegesen telítetlen, adott esetbenlegfeljebb három heteroatomot tartalmazó, öt- vagy hattagú gyűrűtképez, amely adott esetben halogénatommal, oxo- vagy -R8 csoporttalszubsztituált; Rx és Ry -T-R3 csoport, vagy Rx és Ry a közöttük lévőatomokkal együtt egy kondenzált, telítetlen vagy részlegesentelítetlen, adott esetben legfeljebb három heteroatomot tartalmazó, 5-8 tagú gyűrűt képez, amelyben az Rx és Ry által képezett kondenzáltgyűrűben bármely szubsztituálható szénatom oxo- vagy -T-R3 csoporttalszubsztituált, és az Rx és Ry által képezett kondenzált gyűrűbenbármely szubsztituálható nitrogénatom -R4 csoporttal szubsztituált; Tvegyértékkötés vagy alkilidénlánc; R2 és R2' -R vagy -T-W-R6 csoport,vagy R2 és R2' a közöttük lévő atomokkal együtt egy kondenzált,telítetlen vagy részlegesen telítetlen, adott esetben legfeljebb háromheteroatomot tartalmazó, 5-8 tagú gyűrűt képez, amelyben az R2 és R2'által képezett kondenzált gyűrűben bármely szubsztituálható szénatomhalogénatommal, oxo-, ciano-, nitro-, -R7 vagy -V-R6 csoporttalszubsztituált, és az R2 és R2' által képezett kondenzált gyűrűbenbármely szubsztituálható nitrogénatom -R4 csoporttal szubsztituált; R3halogénatom, -R, -OR, -C(=O)R, -CO2R, -COCOR, -COCH2COR, nitro-,ciano-, -S(O)R, -S(O)2R, -N(R7)COR, -N(R7)COO (adott esetbenszubsztituált alifás), -N(R4)N(R4)2, -C=NN(R4)2, -C=N-OR, -N(R7)CON(R7)2 , -N(R7)SO2N(R7)2, -N(R4)SO2R vagy -OC(=O) N(R7)2csoport; R hidrogénatom vagy egy adott esetben szubsztituált alifás,aril-, heteroaril- vagy heterociklilcsoport; W -C(R6)2O-, -C(R6)2S-, -C(R6)2SO-, -C(R6)2SO2-, -C(R6)2SO2-N(R6)-, -C(R6)2N(R6)-, -CO-, -CO2-,-C(R6)OC(O)-, -C(R6)O-C(O)N(R6)-, -C(R6)2N(R6)CO-, -C(R6)2N(R6)C(O)O-,-C(R6)=N-N(R6)-, -C(R6)=N-O-, -C(R6)2N(R6)N(R6)-, -C(R6)2N(R6)SO2-N(R6)-, -C(R6)2N(R6)-CON(R6)- vagy -CON(R6)- csoport; R6 hidrogénatomvagy adott esetben szubsztituált alifás csoport, vagy két ugyanazon anitrogénatomon lévő R6 csoport a nitrogénatommal heterociklil- vagyheteroarilcsoportot képez a vegyületeket tartalmazógyógyszerkészítményekre, valamint a vegyületek alkalmazási eljárásairavonatkozik. ÓThe invention relates to compounds of the general formula that function as protein kinase, especially GSK-3 and Aurora-2 protein kinase inhibitors - in which ring C is a phenyl, pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl or 1,2,4-triazinyl group, where the C ring is a or carries two -R1 ortho-substituents, any other carbon position on the C ring is substituted with an R5 group, and optionally the two adjacent substituents on the C ring together with the atoms between them are monocondensed, unsaturated or partially unsaturated, optionally containing up to three heteroatoms, five- or forms a six-membered ring, optionally substituted with a halogen atom, oxo- or -R8 group; Rx and Ry -T-R3 group, or Rx and Ry together with the atoms between them, form a condensed, unsaturated or partially unsaturated, optionally containing up to three heteroatoms, 5-8 membered ring, in which any substitutable carbon atom in the condensed ring formed by Rx and Ry is oxo - or -T-R3 is subsubstituted, and any substitutable nitrogen atom in the condensed ring formed by Rx and Ry is substituted with -R4; Bivalent bond or alkylidene chain; R2 and R2' -R or -T-W-R6 group, or R2 and R2' together with the atoms between them form a condensed, unsaturated or partially unsaturated, optionally containing up to three heteroatoms, 5-8 membered ring, in which R2 and R2' in the condensed ring formed by any substitutable carbon atom substituted by a halogen atom, oxo-, cyano-, nitro-, -R7 or -V-R6 group, and any substitutable nitrogen atom in the condensed ring formed by R2 and R2' substituted by -R4 group; R3halogen atom, -R, -OR, -C(=O)R, -CO2R, -COCOR, -COCH2COR, nitro-, cyano-, -S(O)R, -S(O)2R, -N(R7) COR, -N(R7)COO (optionally substituted aliphatic), -N(R4)N(R4)2, -C=NN(R4)2, -C=N-OR, -N(R7)CON(R7) 2 , -N(R7)SO2N(R7)2, -N(R4)SO2R or -OC(=O) N(R7)2 group; R is a hydrogen atom or an optionally substituted aliphatic, aryl, heteroaryl or heterocyclyl group; W -C(R6)2O-, -C(R6)2S-, -C(R6)2SO-, -C(R6)2SO2-, -C(R6)2SO2-N(R6)-, -C(R6 )2N(R6)-, -CO-, -CO2-,-C(R6)OC(O)-, -C(R6)O-C(O)N(R6)-, -C(R6)2N(R6) CO-, -C(R6)2N(R6)C(O)O-,-C(R6)=N-N(R6)-, -C(R6)=N-O-, -C(R6)2N(R6)N (R6)-, -C(R6)2N(R6)SO2-N(R6)-, -C(R6)2N(R6)-CON(R6)- or -CON(R6)- group; R6 is a hydrogen atom or optionally substituted aliphatic group, or two R6 groups on the same nitrogen atom form a heterocyclyl or heteroaryl group with the nitrogen atom for pharmaceutical preparations containing the compounds, as well as the methods of application of the compounds. HE

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